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Start Over Author "Stephen T, Wrobleski" Journal organic process research & development
1 results on '"Stephen T, Wrobleski"'

1. Development of a Practical Synthesis of a p38 Kinase Inhibitor via a Safe and Robust Amination

Author

Wendel W. Doubleday, Srinivas Tummala, Simon Leung, Susanne Kiau, Konstantinos Dambalas, Alaric J. Dyckman, Stephen T. Wrobleski, Luca Parlanti, Ehrlic Lo, Hong Wu, Katerina Leftheris, John Hynes, Paul C. Lobben, Zhongping Shi, and Robert P. Discordia

Subjects
chemistry.chemical_compound, Hydroxylamine, chemistry, Organic Chemistry, Organic chemistry, Physical and Theoretical Chemistry, Amination
Abstract

The development of a practical synthesis for a p38 kinase inhibitor is described. The key advances include an improved route to the key intermediate, a substituted pyrrole, and a subsequent animation utilizing O-(4-nitrobenzoyl)hydroxylamine, which provides a safe, scalable, and robust amination method. The new protocol was successfully demonstrated to generate 1.6 kg of API in seven steps and 26% overall yield.

Published
2012
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